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Ananya Deb, Nirmala Grace Andrews, Vimala Raghavan
The present study focuses on the development of a chitosan functionalized nanobiocomposite for the co-delivery of two anti-cancer drugs camptothecin (CPT) and 3,3'‑Diindolylmethane (DIM). The difference in the mechanism of action of the two drugs makes them a promising candidate to produce a synergistic effect against breast cancer. Herein a nanobiocomposite was developed by functionalizing a natural polymer chitosan to graphene oxide nanoparticles and decorated with folic acid. The nanobiocomposite thus synthesized was loaded with camptothecin and 3,3'‑Diindolylmethane and characterized by X-ray diffractometer (XRD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), transmission electron microscopy (TEM), UV-visible spectroscopy (UV) and atomic force microscopy (AFM)...
February 26, 2018: International Journal of Biological Macromolecules
Md Junaid, Raju Dash, Nazrul Islam, Jui Chowdhury, Md Jahangir Alam, Saikat Dev Nath, Mohammad Abu Sayem Shakil, Ashifa Azam, Syed Mustyen Quader, S M Zahid Hosen
Objective: In recent decades, the overexpression of microRNA-21 (miR-21) is found to be progressively linked with many diseases such as different types of cancers, cardiovascular diseases, and inflammation. Thereby, it has become an attractive target for pharmacological and genetic modulation in various diseases, and also for overcoming the resistance to chemotherapy in several cancers. Here, in this study, the role of molecular therapeutics of 3,3'-diindolylmethane (DIM) has been investigated for its ability to bind with the precursor miRNA as a target of miR-21 (hsa-mir-21), which may alter the catalyzation process of dicer, a RNase III enzyme, involved in miRNA transcription...
October 2017: Journal of Pharmacy & Bioallied Sciences
Jae-Rim Heo, Geum-A Lee, Gyu-Sik Kim, Kyung-A Hwang, Kyung-Chul Choi
BACKGROUND: Phytochemicals are derived from plants, vegetables and daily products and exert chemopreventive effects. Malignant melanoma is highly metastatic, and melanoma patients can develop chemotherapeutic resistance against conventional melanoma therapies. METHODS: In the present study, we investigated the anti-cancer effect of the phytochemicals kaempferol (Kaem), genistein (Gen), and 3'3-diindolylmethane (DIM) on melanoma cell viability. We also evaluated the altered expression of cell cycle-related genes...
January 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Thomas T Y Wang, Quynhchi Pham, Young S Kim
Modulation of the immune system by cancer protective food bioactives has preventive and therapeutic importance in prostate cancer, but the mechanisms remain largely unclear. The current study tests the hypothesis that the diet-derived cancer protective compounds, indole-3-carbinol (I3C) and 3,3'-diindolylmethane (DIM), affect the tumor microenvironment by regulation of inflammatory responses in monocytes and macrophages. We also ask whether I3C and DIM act through the aryl hydrocarbon (AHR)-dependent pathway or the signaling lymphocyte activation molecule (SLAM) family protein CD84-mediated pathway...
January 24, 2018: International Journal of Molecular Sciences
Mingli Su, Chenchen Qian, Yumin Hu, Wenhua Lu, Rongkang Huang, Minhu Chen, Jie Chen
3'3-Diindolylmethane (DIM) has been proved to exhibit anticancer properties in many solid tumors. In our previous study, we demonstrated that DIM inhibited SGC7901 cell proliferation by inducing apoptosis and delaying cell cycle progression. Herein, we further explored the anti-tumor effect of DIM on SGC-7901 tumor bearing mice. Tumors were excised, weighed, and tested by western blot and TdT-UTP nick-end labeling (TUNEL) assay. Blood samples were collected for biochemical analysis. The expression levels of AhR and cytochrome P450, family 1, subfamily A, polypeptide 1 (CYP1A1) protein were evaluated by western-blot assay...
December 2017: Oncology Letters
Bo-Gyoung Kim, Jin-Wook Kim, Soo-Min Kim, Ryeo-Eun Go, Kyung-A Hwang, Kyung-Chul Choi
Cyprodinil (CYP) is a pyrimidine amine fungicide that has been extensively used in agricultural areas. 3,3'-Diindolylmethane (DIM) is a derivative of the dietary phytoestrogen, indole-3-carbinol (I3C), which is derived from cruciferous vegetables and considered to be a cancer-preventive phytonutrient agent. In this study, the effects of CYP and DIM were examined on the cell viability, invasion, and metastasis of human endometrial cancer cells, Ishikawa, via epithelial mesenchymal transition (EMT). CYP increased the level of cell viability of Ishikawa cells compared to DMSO as a control, as did E2...
January 8, 2018: International Journal of Molecular Sciences
Geum-A Lee, Kyung-Chul Choi, Kyung-A Hwang
Triclosan (TCS) and bisphenol A (BPA) are endocrine-disrupting chemicals that interfere with the hormone or endocrine system and may cause cancer. Kaempferol (Kaem) and 3,3'-diindolylmethane (DIM) are phytoestrogens that play chemopreventive roles in the inhibition of carcinogenesis and cancer progression. In this study, the influence of TCS, BPA, Kaem, and DIM on proliferation and apoptotic abilities of VM7Luc4E2 breast cancer cells were examined. MTT assay revealed that TCS (0.1-10 μM), BPA (0.1-10 μM) and E2 (0...
January 9, 2018: Biomolecules & Therapeutics
Elsa N Garza-Trevino, Martha S Rodriguez-Gonzalez, Paulina Delgado Gonzalez, Yesenia G Alonso-Cruz, Yesenia G Alonso-Cruz, Adolfo Soto-Dominguez, Juan F Gonzalez Guerrero, Yanko Castro-Govea, Emiliano Michel Sanchez, Salvador Said Fernandez, Herminia G Martinez-Rodriguez
PURPOSE: To determine in vitro, the efficacy and safety window of not-front-line and first-line anti-colorectal (CRC) drug combinations. METHODS: The adenocarcinoma cell line Colo 320DM and normal human mesenchymal stem cells derived from adipose tissue were used respectively to determine the anti-CRC efficacy (% of Colo 320DM cell death [CD]) and safety window [SW] - % Colo 320DM percent cancer death (PCD)/% of mesenchymal stem cell's death) of drug combinations, using the adenosine triphosphate-based chemotherapy response assay (ATP-CRA)...
September 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
O L Zinovieva, E N Grineva, M M Prokofjeva, D S Karpov, G S Krasnov, V S Prassolov, T D Mashkova, N A Lisitsyn
Using real-time RT-PCR in combination with bioinformatics, we have shown for the first time that the treatment of HCT-116 and HT-29 colon cancer cells with two anti-cancer agents (doxycycline or 3,3'-diindolylmethane) results in profound changes in the intracellular content of several lncRNAs (by up to 100 times). Since many of these RNAs are secreted by tumors into the bloodstream, the obtained results provide a basis for developing more sensitive protocols for serological monitoring of tumor relapse and metastasis, as well as for search of new anti-cancer drugs...
September 2017: Molekuliarnaia Biologiia
Amira Jalil Fragoso-Medina, René Gerardo Escobedo-González, María Inés Nicolás-Vázquez, Gabriel Arturo Arroyo-Razo, María Olivia Noguez-Córdova, René Miranda-Ruvalcaba
The structure of the ortho-, meta- and para- hybrid diindolylmethane-phenylboronic acids and their interactions were optimized with by a quantum chemical method, using density functional theory at the (DFT) level. Thus, infrared bands were assigned based on the scaled theoretical wavenumbers by correlating the respective experimental data of the molecules. In addition, the corresponding ¹H-/(13)C-/(11)B-NMR experimental and theoretical chemical shifts were correlated. The target molecules showed a poor treatment of the OH shifts in the GIAO method due to the absence of explicit solvent effects in these calculations; therefore, they were explicitly considered with acetone molecules...
October 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Kai Liang, Wen-Hao Qian, Jing Zong
Autophagy is activated in the ischemic heart and is a process that is essential for survival, differentiation, development and homeostasis. 3,3'‑Diindolylmethane (DIM) is a natural product of the acid‑catalyzed condensation of indole‑3‑carbinol in cruciferous vegetables. Numerous studies have suggested that DIM has various pharmacological effects, including antioxidant, antitumor, anti‑angiogenic and anti‑apoptotic properties. However, the function of DIM on hypoxia‑induced cardiac injury remains to be elucidated...
December 2017: Molecular Medicine Reports
Arijit Bhowmik, Sayak Chakravarti, Aparajita Ghosh, Rajni Shaw, Suman Bhandary, Satyaranjan Bhattacharyya, Parimal C Sen, Mrinal K Ghosh
Current therapy for Glioblastoma is insufficient because of the presence of blood brain barrier. It limits the transport of essential drugs to the tumor sites. To overcome this limitation we strategized the delivery of an anticancer compound 3,3'-diindolylmethane by encapsulation in poly (lactic-co-glycolic acid) nanoparticles. These nanoparticles were tagged with a novel peptide against somatostatin receptor 2 (SSTR2), a potential target in glioma. The nanoformulation (27-87nm) had loading and encapsulation efficiency of 7...
September 12, 2017: Oncotarget
Abdullah M Alzahrani, Hamza Hanieh, Hairul-Islam Mohamed Ibrahim, Omar Mohafez, Tamer Shehata, Mohammad Bani Ismail, Manal Alfwuaires
BACKGROUND: Chronic inflammation in ulcerative colitis (UC) patients is the major risk factor for colitis-associated colon cancer (CAC). Recent evidences have shown that microRNAs (miRNAs) are implicated in CAC pathogenesis. However, the interaction of miRNAs with the transcription factors that alleviate CAC has not been reported. METHODS: 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or 3,3'-diindolylmethane (DIM) were used to activate aryl hydrocarbon receptor (Ahr) in azoxymethane (AOM)/dextran sodium sulfate (DSS)-induced CAC in mice...
October 7, 2017: International Immunopharmacology
Alfonso Lopez-Vazquez, Jesus J Garcia-Banuelos, Angelica S Gonzalez-Garibay, Pedro E Urzua-Lozano, Susana Del Toro-Arreola, Miriam R Bueno-Topete, Sergio Sanchez-Enriquez, Jose F Munoz-Valle, Luis F Jave-Suarez, Juan Armendariz-Borunda, Blanca E Bastidas-Ramirez
BACKGROUND: 3,3'-Diindolylmethane (DIM) is a condensation product of indole-3-carbinol, a glucosinolate naturally occurring in Brassica genus vegetables. The antiinflammatory properties of DIM through the inhibition of NF-κB, as well as its ameliorating effects on glucose tolerance and hyperglicemic states, have been described. A subclinical proinflammatory profile resultant from the interaction of adipocytes and macrophages has been reported in obesity, affecting the insulin signaling pathway, contributing to insulin resistance...
2017: Medicinal Chemistry
Hossam Draz, Alexander A Goldberg, Vladimir I Titorenko, Emma S Tomlinson Guns, Stephen H Safe, J Thomas Sanderson
3,3'-Diindolylmethane (DIM) and its synthetic halogenated derivatives 4,4'-Br2- and 7,7'-Cl2DIM (ring-DIMs) have recently been shown to induce protective autophagy in human prostate cancer cells. The mechanisms by which DIM and ring-DIMs induce autophagy have not been elucidated. As DIM is a mitochondrial ATP-synthase inhibitor, we hypothesized that DIM and ring-DIMs induce autophagy via alteration of intracellular AMP/ATP ratios and activation of AMP-activated protein kinase (AMPK) signaling in prostate cancer cells...
December 2017: Cellular Signalling
Subhadip Hajra, Abhishek Basu, Somnath Singha Roy, Arup Ranjan Patra, Sudin Bhattacharya
The most crucial complication related to doxorubicin (DOX) therapy is nonspecific cytotoxic effect on healthy normal cells. The clinical use of this broad-spectrum chemotherapeutic agent is restricted due to development of severe form of cardiotoxicity, myelosuppression, and genotoxicity which interfere with therapeutic schedule, compromise treatment outcome and may lead to secondary malignancy. 3,3'-diindolylmethane (DIM) is a naturally occurring plant alkaloid formed by the hydrolysis of indolylmethyl glucosinolate (glucobrassicin)...
October 2017: Free Radical Research
Nieves Baenas, Clara Suárez-Martínez, Cristina García-Viguera, Diego A Moreno
The evaluation of the bioavailability of bioactive compounds from cruciferous foods is one challenge in the design of clinical trials for studying their functionality. Currently, studies of bioavailability are mainly based of the analysis of total isothiocyanates and indoles, and sulforaphane metabolites after broccoli consumption. However, as far as we are aware, there are not any biomarkers studied or established for the intake of radish sprouts. In this work, a 7-days-cross-over study with fourteen women was undertaken to compare the bioavailability of glucosinolates from broccoli and radish sprouts...
October 2017: Food Research International
Geum-A Lee, Kyung-A Hwang, Kyung-Chul Choi
As a phytoestrogen, 3,3'-diindolylmethane (DIM) plays a chemopreventive role by inhibiting cancer progression. In this study, we examined the effects of 17β-estradiol (E2), two endocrine disrupting chemicals (EDCs), triclosan (TCS) and bisphenol A (BPA), and DIM on epithelial-mesenchymal transition (EMT) and metastatic behaviors of estrogen receptor (ER)-positive MCF-7 breast cancer cells. An in vitro assay revealed that E2 (10(-9) M), TCS (10(-5)-10(-7) M), and BPA (10(-5)-10(-7) M) induced MCF-7 cell proliferation compared to a control through the ER pathway...
August 24, 2017: Food and Chemical Toxicology
Md Abu Sayeed, Massimo Bracci, Guendalina Lucarini, Raffaella Lazzarini, Roberto Di Primio, Lory Santarelli
Malignant mesothelioma (MM) is a very aggressive, lethal cancer, and its incidence is increasing worldwide. Development of multi-drug resistance, therapy related side-effects, and disease recurrence after therapy are the major problems for the successful treatment of MM. Emerging evidence indicates that dietary phytochemicals can exert anti-cancer activities by regulating microRNA expression. Until now, only one dietary phytochemical (ursolic acid) has been reported to have MM microRNA regulatory ability. A large number of dietary phytochemicals still remain to be tested...
October 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Anirban Kayet, Vinod K Singh
A Pd(ii)-Ag(i) catalyzed highly efficient synthesis of diindolylmethane has been developed. This transformation consists of a one-pot sequential Sonogashira coupling (and desilylation) followed by cycloisomerization/C3-functionalization of 2-iodoanilines. Six new bonds (four C-C and two C-N) are formed in a one-pot fashion. A variety of diindolylmethanes were obtained in excellent yields (up to 94%) under mild reaction conditions and this strategy is amenable to gram scale synthesis also. The products were transformed into various synthetically useful compounds...
August 23, 2017: Organic & Biomolecular Chemistry
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